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Compound Detail

CHEMBL242711

BERGAPTOL
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O=c1ccc2c(O)c3ccoc3cc2o1

Basic Information

ChEMBL ID CHEMBL242711
Name BERGAPTOL
Phase Preclinical
Structure Type MOL
InChI Key GIJHDGJRTUSBJR-UHFFFAOYSA-N
3
Targets
3
Activities
2
Assay Types
0
PK Parameters
12
Publications
0
Known Names

Molecular Properties

202.2
MW (Da)
2.24
ALogP
4
HBA
1
HBD
63.6
PSA (Ų)
0.57
QED
0
Ro5 Violations
0
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

Natural Product First in Class Prodrug

Extended Properties

Molecular Formula C11H6O4
MW 202.16
Aromatic Rings 3
Heavy Atoms 15
NP-Likeness 1.03

Activity Summary

IC50 2 meas. best 4.6
Ki 1 meas. best 4.94

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cytochrome P450 2A6
CHEMBL5282
Ki 4.94 4.94 11600.0 1
Cytochrome P450 3A4
CHEMBL340
IC50 4.6 4.6 24920.0 1
Unchecked
CHEMBL612545
IC50 4.38 4.38 41500.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
17400460 10.1016/j.bmc.2007.03.047 NON-PROTEIN TARGET 2
17400460 10.1016/j.bmc.2007.03.047 Cytochrome P450 3A4 2
17400460 10.1016/j.bmc.2007.03.047 No relevant target 2
16248836 10.2174/138920005774330639 Cytochrome P450 2A6 2
22222157 10.1016/j.bmc.2011.12.002 Beta-secretase 1 2
23291118 10.1016/j.ejmech.2012.11.043 Radical scavenging activity 2
19054677 10.1016/j.bmc.2008.11.039 HT-29 1
19054677 10.1016/j.bmc.2008.11.039 3T3-L1 1
10903978 10.1038/sj.bjp.0703433 ATP-dependent translocase ABCB1 1
23291118 10.1016/j.ejmech.2012.11.043 No relevant target 1
23291118 10.1016/j.ejmech.2012.11.043 Unchecked 1
26112067 10.1016/j.ejmech.2015.06.017 Mycobacterium tuberculosis 1

Data from ChEMBL 36 via Core Engine